US10052322B2ActiveUtilityA1
Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one
Est. expiryApr 17, 2033(~6.8 yrs left)· nominal 20-yr term from priority
A61K 9/2054A61K 9/2018A61K 31/4985A61K 9/4858C07D 471/04C07D 487/04A61P 35/00C07D 403/14C07D 401/14
65
PatentIndex Score
0
Cited by
237
References
18
Claims
Abstract
Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1. A pharmaceutical composition comprising 1-ethyl-7-(2-methyl-6-(4H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, or a pharmaceutically acceptable salt, tautomer, isotopologue or stereoisomer thereof, and mannitol, microcrystalline cellulose, sodium starch glycolate, silicon dioxide, stearic acid, ethylenediaminetetraacetic acid disodium salt dihydrate, and magnesium stearate.
2. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises about 10% by weight of 1-ethyl-7-(2-methyl-6-(4H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, or a pharmaceutically acceptable salt, tautomer, isotopologue or stereoisomer thereof.
3. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises about 25% by weight of microcrystalline cellulose.
4. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises about 3% by weight of sodium starch glycolate.
5. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises about 0.5% by weight of ethylenediaminetetraacetic acid disodium salt dihydrate.
6. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises about 10% by weight of 1-ethyl-7-(2-methyl-6-(4H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, or a pharmaceutically acceptable salt, tautomer, isotopologue or stereoisomer thereof, about 25% by weight of microcrystalline cellulose, about 3% by weight of sodium starch glycolate, about 0.5% by weight of ethylenediaminetetraacetic acid disodium salt dihydrate and about 0.65% by weight of magnesium stearate.
7. A method for treating a cancer, comprising administering to a patient having a cancer the pharmaceutical composition of claim 1 ,
wherein the cancer is glioblastoma multiforme, head and neck squamous cell carcinoma, castration-resistant prostate cancer, Ewing's sarcoma, chronic lymphocytic leukemia or small lymphocytic lymphoma.
8. The method of claim 7 , wherein the cancer is glioblastoma multiforme.
9. The method of claim 8 , wherein the glioblastoma multiforme is characterized by O6-methylguanine-DNA methyltransferase (MGMT) methylation.
10. The method of claim 7 , wherein the cancer is head and neck squamous cell carcinoma.
11. The method of claim 10 , wherein the head and neck squamous cell carcinoma is characterized by deletion of chromosome 11q22 or loss of ataxia telangiectasia mutated (ATM) expression.
12. The method of claim 7 , wherein the cancer is castration-resistant prostate cancer.
13. The method of claim 12 , wherein the castration-resistant prostate cancer is E-twenty six (ETS) overexpressing castration-resistant prostate cancer.
14. The method of claim 7 , wherein the cancer is Ewing's sarcoma.
15. The method of claim 14 , wherein the Ewing's sarcoma is E-twenty six (ETS) overexpressing Ewings sarcoma.
16. The method of claim 7 , wherein the cancer is chronic lymphocytic leukemia.
17. The method of claim 16 , wherein the chronic lymphocytic leukemia is characterized by deletion of chromosome 11q22, loss of ataxia telangiectasia mutated (ATM) expression, mutation of IgVH, wild type IgVH, wild type p53/ATM, mutation of p53 or dysfunctional p53.
18. The method of claim 7 , wherein the cancer is small lymphocytic lymphoma.Cited by (0)
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